Abstract
This study aimed to optimize and evaluate self-assembled liquid crystalline nanoparticles (SALCs) prepared from phospholipids and oleic acid for enhancing the absorption of Ω-3s. We explored the structure and optimal formulation of SALCs, which are composed of Ω-3 ethyl ester (Ω-3 EE), phospholipids, and oleic acid, using a ternary diagram and evaluated the improvement in Ω-3 dissolution, permeation, and oral bioavailability. The in vitro dissolution and pharmacokinetics of Ω-3 SALCs were compared with those of Omacor soft capsules (as the reference). The shape of the liquid crystal was determined according to the composition of phospholipids, oleic acids, and Ω-3s and was found to be in cubic, lamellar, and hexagonal forms. The dissolution rates of eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) obtained from Ω-3 SALCs were 1.7 to 2.3-fold higher than those of the Omacor soft capsules. Furthermore, a pharmacokinetic study in male beagle dogs revealed that Ω-3 SALCs increased the oral bioavailability of Ω-3 EE by 2.5-fold for EPA and 3.1-fold for DHA compared with the reference. We found an optimal formulation that spontaneously forms liquid crystal-based nanoparticles, improving the bioavailability of EPA and DHA, not found in the existing literature. Our findings offer insight into the impact of nanoparticle phase on the oral delivery of oil-soluble drugs and provide a novel Ω-3 EE formulation that improves the bioavailability of EPA and DHA.
Highlights
Accepted: 20 December 2021The Ω-3s, known as n-3 polyunsaturated fatty acids (PUFAs), are essential fatty acids and important cell membrane components [1]
Phospholipids were selected as vital components to form liquid crystals for establishing self-assembled liquid crystalline nanoparticles (SALCs) with Ω-3
3.1-fold higher than the 2308.63 ± 937.07 ng/mL and 7130.45 ± 3421.18 ng·h/mL for the reference sample, respectively. These results showed that SALC formulations successfully enhanced the bioavailability of Ω-3 Ω-3 ethyl ester (EE) because of the improvement in dissolution and permeation, resulting in the formation of a cubic structure, which spontaneously formed nanoparticles of the smallest size in the GI tract and improved the solubility and dissolution of Ω-3 ethyl ester (Ω-3 EE) (Figure 7)
Summary
Accepted: 20 December 2021The Ω-3s, known as n-3 polyunsaturated fatty acids (PUFAs), are essential fatty acids and important cell membrane components [1]. The administration of Ω-3 fatty acids is a remedial treatment for cardiovascular diseases and depressive disorders in adults [3,4,5,6,7]. The Ω-3 ethyl esters (Ω-3 EE) of Ω-3 fatty acids are used as a prescription drug approved by the FDA to treat hypertriglyceridemia in most cardiovascular diseases and have a strong safety profile when taken as directed. The long-chain fatty acids EPA and DHA have been found to be absorbed by the gastrointestinal (GI) tract in their free form effectively [12,13,14,15,16]; their original molecules enter the micelles independently and are taken up by enterocytes through diffusion or transport systems along with CD36/FABP
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